SALAGEN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SALAGEN (SALAGEN).
Pilocarpine is a cholinergic parasympathomimetic agent that acts as a muscarinic receptor agonist, stimulating exocrine gland secretion (salivary, sweat, lacrimal, gastric, pancreatic) and smooth muscle contraction.
| Metabolism | Primarily metabolized by hepatic esterases and microsomal enzymes; undergoes first-pass metabolism; metabolites are inactive and excreted renally. |
| Excretion | Renal excretion of unchanged drug and metabolites: 80-90% in urine, with approximately 20% unchanged; biliary/fecal excretion accounts for less than 5%. |
| Half-life | Terminal elimination half-life is 5-6 hours in patients with normal renal function; may be prolonged to 6-8 hours in elderly or those with hepatic impairment. |
| Protein binding | Approximately 30% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is approximately 2-4 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral bioavailability is about 100% due to complete absorption from the gastrointestinal tract. |
| Onset of Action | Oral: Onset of salivary flow occurs within 30 minutes; peak effect at 1-2 hours. |
| Duration of Action | Duration of saliva stimulation is 3-5 hours after a single oral dose; clinical effect may persist up to 6 hours. |
5 mg orally three times daily.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment recommended for mild to moderate renal impairment; contraindicated in severe renal impairment (CrCl < 10 mL/min). |
| Liver impairment | Contraindicated in Child-Pugh class C cirrhosis; use with caution in Child-Pugh class A or B, starting at 5 mg twice daily and titrating cautiously. |
| Pediatric use | Not approved for use in pediatric patients; safety and efficacy not established. |
| Geriatric use | Start with 5 mg twice daily due to increased risk of adverse effects (e.g., excessive sweating, bradycardia); titrate slowly based on response and tolerability. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SALAGEN (SALAGEN).
| Breastfeeding | Unknown if excreted in human milk. Caution advised; consider benefit to mother versus risk to infant. |
| Teratogenic Risk | Pregnancy Category C. No adequate human studies; animal studies show no teratogenicity at clinically relevant doses. Risk cannot be ruled out; use only if benefit outweighs potential risk. |
| Fetal Monitoring | Monitor for cholinergic effects (bradycardia, hypotension, bronchospasm) in mother and fetus. Fetal heart rate monitoring recommended. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to pilocarpine or any component","Acute iritis or angle-closure glaucoma (may worsen condition)","Uncontrolled asthma","Severe cardiovascular disease (e.g., bradycardia, hypotension)"]
| Precautions | ["Use with caution in patients with cardiovascular disease (bradycardia, hypotension, hypertension, arrhythmias)","Avoid in patients with uncontrolled asthma or COPD (may exacerbate bronchospasm)","May cause visual disturbances (miosis, blurred vision) especially at night","Risk of excessive sweating, dehydration, and electrolyte imbalance","Use with caution in patients with biliary tract disease or renal impairment"] |
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| Fertility Effects | No known effect on fertility in humans; animal studies show no impairment. |